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Anti-breast cancer potential of SS5020, a novel benzopyran antiestrogen

✍ Scribed by Naomi Suzuki; Xiaoping Liu; Y. R. Santosh Laxmi; Kanako Okamoto; Hyo Jeong Kim; Guangxiang Zhang; John J. Chen; Yoshinori Okamoto; Shinya Shibutani

Publisher
John Wiley and Sons
Year
2010
Tongue
French
Weight
608 KB
Volume
128
Category
Article
ISSN
0020-7136

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✦ Synopsis

Abstract

Treatment with tamoxifen (TAM) increases the risk of developing endometrial cancer in women. The carcinogenic effect is thought to involve initiation and/or promotion resulting from DNA damage induced by TAM as well as its estrogenic action. To minimize this serious side‐effect while increasing the anti‐breast cancer potential, a new benzopyran antiestrogen, 2E‐3‐{4‐[(7‐hydroxy‐2‐oxo‐3‐phenyl‐2H‐chromen‐4‐yl)‐methyl]‐phenyl}‐acrylic acid (SS5020), was synthesized. Unlike TAM, SS5020 exhibits no genotoxic activity to damage DNA. Furthermore, SS5020 does not present significant uterotrophic potential in rats; in contrast, the structurally related compounds, TAM, toremifene, raloxifene (RAL) and SP500263 all have uterotrophic activity. At the human equivalent molar dose of TAM (0.33 or 1.0 mg/kg), SS5020 had much stronger antitumor potential than those same antiestrogens against 7,12‐dimethylbenz(a)anthracene‐induced mammary carcinoma in rats. The growth of human MCF‐7 breast cancer xenograft implanted into athymic nude mice was also effectively suppressed by SS5020. SS5020, lacking genotoxic and estrogenic actions, could be a safer and stronger antiestrogen alternative to TAM and RAL for breast cancer therapy and prevention.

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